New highly hydrosoluble and not self-aggregated perylene derivatives with three and four polar side-chains as G-quadruplex telomere targeting agents and telomerase inhibitors

Four new perylene derivatives with three and four basic side-chains are reported here as G-quadruplex interactive compounds. The new perylene derivatives are readily soluble in water and not self-aggregated, in contrast to what happens with the previously reported two side-chain perylene derivatives. All four compounds are able to induce the G-quadruplex and to inhibit 50% of telomerase activity at about 5 μM concentration, showing a similar efficiency with respect to each other. Molecular modelling studies are presented to try to explain these findings.

Graphical abstractFour new perylene derivatives with three and four basic side chains, readily soluble in water and not self-aggregated, are presented here. All four compounds are able to inhibit human telomerase and to induce different G-quadruplex structures.Figure optionsDownload full-size imageDownload as PowerPoint slide